Gastric acid binding chewing pastilles

ABSTRACT

The subject matter of the invention is chewing pastilles based on at least partially or complete water soluble natural and/or synthetic polymers, selected from gums, alginates, carrageen, starch, pectin, and gelatin, which will form gels or viscous solutions in aqueous system, and additional adjuvants and additives, said pastilles containing antacids as active ingredients.

The invention relates to chewing pastilles based on certain naturaland/or synthetic polymers comprising antacids as active ingredients.

By the term pastilles there is generally understood--see also W. Rahn,Pharmazeutische Zeitung, pp 2214-2218 (1982)--preparations which can besucked or chewed in the mouth. Namely, it is differentiated essentiallybetween tablets, hard candies and gum pastilles (also designated as gumcandies).

The processes for producing such dosage forms are basicallydistinguished from each other.

Tablets are pressed on tablet machines. To this end, the tablet mass hasto be prepared by mixing and granulating. Several authors already havedealt with granulating methods for active substances which are difficultto process.

Candies are prepared by mixing saccharose and glucose syrup, boiling theresulting mixture at about 130° C., and removing most of the water fromthe mass in vacuo to a residual water content of from 0.5 to 2%. To thehighly viscous candy mass cooled down to about 85° C. are added theactive substances and flavors and admixed by kneading. With continuouscooling, the candy mass is drawn into strands, shaped, and cut intapered rollers and other candy machines. It is known that, due to theviscosity of the candy mass, the distribution of the active substance israther non-uniform.

Gum pastilles are prepared by initially dissolving in an agitator vesselhydrocolloids, e.g., gum arabic, together with saccharose, glucosesyrup, sorbitol, xylitol, and the like in water, and dissolving,emulsifying or suspending the active ingredients in this base mass. Thecasting composition thus obtained is cast into so-called powder trays.These are, for example, flat wooden boxes of about 80×40 cm filled withstarch, especially corn starch. The desired shapes are pressed into thesmoothed powder using a stamp board, and the warm casting solution isexactly metered and pumped into the thus obtained wells, wherein thecast mass is not bound to the powder. Tray by tray, 500 to 1000pastilles each, is thus cast, stacked, and water is removed from thepastilles in drying chambers to about 10% of residual moisture within 3to 4 days. The pastilles thus produced are "depowdered" and thensubjected to a final treatment.

The subject matter of DE 41 40 116 A1 is pastilles based on naturaland/or synthetic polymers or fat-like substances with sugar and/or sugarsubstitutes, comprising poly(dimethyl siloxane) (Dimeticon, Simeticone),and a process for the preparation thereof.

According to Rompp Chemie Lexikon, 9th edition, page 200, 1989, the term"antacids" is used to mean substances which are to counteracthyperacidity of the gastric juice. Suitable compounds include magnesiumhydroxide, magnesium oxide, magnesium carbonate, magnesium silicate,aluminum hydroxides, aluminum phosphate, magnesium aluminum silicates,hydrotalcite and magaldrate. Although, according to Rompp, the use ofthe prior sodium hydrogen carbonate and calcium carbonate should bedesisted from, numerous commercial products are available which containthese components at least in minor proportions.

The object of the present invention as compared to the prior art hasbeen to provide a novel single dosable dosage form of antacids using acasting process per se known from confectionery manufacture, whichdosage form is characterized by: finest distribution of the activeingredient within the pastille, very accurate single dosing of theactive ingredient, very easy handling of the active ingredient,especially convenient intake of the medicament, and optimum sustainingof the active ingredient in the stomach by the pastilles being slowlychewed.

The aforementioned object is achieved by pastilles based on at leastpartially or completely water soluble natural and/or synthetic polymers,selected from gums, alginates, carrageens, starch, pectin, and gelatinwhich form gels or viscous solutions in aqueous systems, and furtheradjuvants and additives, the pastilles containing antacids as activeingredients.

It has been found that the antacids, being in part water soluble and inpart water insoluble, may be incorporated in an extraordinarily simpleway in a finely dispersed form in pastilles based on the natural and/orsynthetic polymers mentioned.

The term "pastilles" and particularly the term "gum pastilles" withinthe meaning of the present invention comprise those which are preparedby casting. Accordingly, the pastilles of the present invention consistof differently shaped elastic molded parts containing antacids in afinest distribution within a mixture of hydrocolloids and otheradjuvants and additives. Gum pastilles are designated as solid solutionswhich upon sucking are retransformed to liquid solutions or dispersions.By means of the present invention, it is possible to achieve an exactsingle dosage of the pastilles with a relatively mild processing of theingredients. With the mentioned, at least partially or completely watersoluble natural and/or synthetic polymers, it is possible to achieve aparticularly good incorporation of antacids as it is possible to work atrelatively low temperatures. Thus, a particularly homogeneousdistribution of the active substance in the total composition is createdallowing the dosage of the active ingredient with standard deviations inthe range of from 0.5 to 2%. In addition, it is possible according tothe process of the present invention to produce antacids pastilleshaving a relatively high concentration.

Especially preferred natural and/or synthetic polymers within themeaning of the present invention are also known by the term of"hydrocolloids". Especially preferred are the gums selected from gumarabic, gelatin and tragacanth. In the same way, adjuvants and additivesare preferably selected from sugar and/or sugar substitutes,hydrogenated fats, stearic acid, paraffins, oligosaccharides,polysaccharides and/or dextran.

Corresponding pastilles with other active substances are per se known inthe prior art by the term of "gum pastilles". This name is derived fromthe raw material, gum arabic, incorporated therein. Also within themeaning of the present invention, this hydrocolloid is preferably usedas a base material since it imparts good sucking and chewing propertiesto the pastilles.

Besides the polymers, the base mass in particular containsflavor-carrying substancves, such as sugar and/or sugar substitutes,since the patient is supposed to chew the pastille. Accordingly, it isnecessary that the pastilles have such a good taste that they are notrefused or swallowed down. To improve the taste, as known as such in theprior art, corresponding adjuvants are used, such as saccharose or itssubstitutes, such as fructose, hydrogenated glucose syrup, sorbitol,mannitol and/or xylitol, as well as known artificial sweeteners. Inaddition, taste corrigents and essences as well as ethereal oils may beused.

The relative amounts of the respectively necessary ingredients of thepastilles are less critical. Accordingly, the base mass contains, forexample, from 2 to 80% by weight of the polymers, based on the totalmass of the pastilles. Especially preferred is an amount of from 10 to60% by weight or gum arabic or from 10 to 60% by weight of gelatin,respectively based on the total mass of the pastilles.

In a further preferred embodiment of the present invention, thepastilles contain from 20 to 50% by weight of sugar and/or sugarsubstitutes, based on the total mass of the pastilles. The amount ofantacids may be varied within a wide range in the inventive pastilles.Preferably, the amount of antacids, based on the total formulation,should be as large as possible, at least to have an acid bindingcapacity of from 20 to 25 mval per unit dose.

Commercially available preparations, such as suspensions or chewingtablets, containing acid-binding active ingredients contain antacidshaving an acid binding capacity of from 10 to 25 mval. Accordingly, aparticularly preferred embodiment of the present invention providespastilles having an acid binding capacity of from 10 to 40 mval.

In the preparation of the pastilles, the above defined polymers, inparticular, are contacted with water and other adjuvants and additivesto form a gel or a viscous solution. Subsequently, antacids aresuspended or dissolved in the base composition thus obtained, and thisliquid composition is then cast into molds, dried either at roomtemperature or at an elevated temperature, especially from 40 to 70° C.,preferably from 40 to 50° C., removed from the mold and subjected tofinal treatment.

For example, at the beginning of the preparation process, gelatin andgum arabic are dissolved in water and suspended together with antacids.This drug mixture is cast into so-called powder trays and dried,separated from the powder and subjected to final treatment as previouslydescribed. The particular advantages of the inventive pastilles and ofthe process for the preparation thereof are a low temperature load ofthe adjuvants and active ingredients, the complete homogeneity thereofin the casting mass which enables the active ingredient to be dosed withhigh accuracy, and most important of all, the excellent chewability ascompared to tablets, and the improved taste, each of which areadvantages promoting the compliance of the patient.

We claim:
 1. Gum pastilles prepared by dissolving in water at leastpartially or completely water soluble natural and/or synthetic polymersselected from the group consisting of gums, alginates, carrageen,starch, and pectin, which polymers are hydrocolloids and form gels orviscous solutions in aqueous systems, and additional adjuvants andadditives, and dissolving, emulsifying, or suspending antacids into theresulting solution such that said antacids are homogeneously distributedin the pastille, said antacids having an acid binding capacity of from10 to 40 mval per unit dose wherein the pastilles comprise from 2 to 80%by weight of the polymers based on the total mass of the pastilles. 2.The pastilles according to claim 1 wherein the chewing pastilles arebased on at least gums selected from gum arabic or tragacanth.
 3. Thepastilles according to claim 1 wherein the adjuvants and additives areselected from the group consisting of sugar, sugar substitutes,hydrogenated fats, stearic acid, paraffins, oligosaccharides,polysaccharides, dextran, and mixtures thereof.
 4. The pastillesaccording to claim 3 comprising sugar substitutes selected from thegroup consisting of fructose, sorbitol, mannitol, xylitol, hydrogenatedglucose syrup, artificial sweeteners, and mixtures thereof.
 5. Thepastilles according to claim 2 wherein the pastilles comprise from 10 to60% by weight of gum arabic based on the total mass of the pastilles. 6.The pastilles according to claim 4 wherein the pastilles comprise from20 to 50% by weight of sugar substitutes based on the total mass of thepastilles.
 7. The pastilles according to claim 1 wherein the antacidshave an acid binding capacity from 10 to 25 mval per unit dose.
 8. Thepastilles according to claim 1 wherein the antacids are selected fromthe group consisting of aluminum hydroxides, aluminum phosphates,magnesium hydroxide, magnesium oxide, magnesium carbonate, magnesiumsilicate, magnesium aluminum silicates, hydrotalcite and magaldrate,sodium carbonate, calcium carbonate, and mixtures thereof.